- Synthesis of 1,4-Dicarbonyl Compounds by Visible-Light-Mediated Cross-Coupling Reactions of α-Chlorocarbonyls and Enol Acetates
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Herein, we report a protocol for visible-light-mediated radical coupling reactions of α-chloroketones and enol acetates to afford 1,4-dicarbonyl compounds, which are important precursors and intermediates in organic synthesis. The reaction involves photoredox-catalyzed activation of the α-chloroketone upon photoelectron transfer, carbon–chlorine bond cleavage, and coupling of the resulting radical with the carbon–carbon double bond of the enol acetate. This mild protocol has a wide substrate scope and moderate to good yields. (Figure presented.).
- Liu, Qiang,Wang, Rui-Guo,Song, Hong-Jian,Liu, Yu-Xiu,Wang, Qing-Min
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supporting information
p. 4391 - 4396
(2020/09/21)
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- Alpha-amino acid derivative containing piperidine thiazole heterocycle and preparation method and application of alpha-amino acid derivative
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The invention discloses an alpha-amino acid derivative containing piperidine thiazole heterocycle. The alpha-amino acid derivative has a structural formula of formula I shown in the description, wherein in formula I, Ar is a phenyl group or a substituted phenyl group, a substituted group of the substituted phenyl group is one of a trifluoromethyl group, fluorine, chlorine or bromine, and R is oneof H and isopropyl. The invention further discloses a preparation method of the alpha-amino acid derivative and application of the alpha-amino acid derivative serving as an insecticide to prevention and control of armyworms. The novel alpha-amino acid derivative containing the piperidine thiazole heterocycle is simple in preparation method, can be used for prevention and control of armyworm insectpests, particularly has a good insecticidal activity against the armyworms, and provides bases for research and development of amino acid pesticides.
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Paragraph 0024
(2019/02/27)
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- A Simple and Efficient Method for the Preparation of α-Halogenated Ketones Using Iron(III) Chloride and Iron(III) Bromide as Halogen Sources with Phenyliodonium Diacetate as Oxidant
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α-Halogenated ketones are both unique structure moieties existing in biologically natural products and valuable synthetic intermediates for the preparation of functional molecules. An efficient and scalable method for the preparation of α-halogenated ketone using iron (III) chloride and iron (III) bromide as halogen sources with phenyliodonium diacetate as oxidant has been developed, featuring mild reaction conditions, environmentally friendly reagents, and wide substrate scope. Notably, the three-step synthesis of drug prasugrel was achieved using this developed method as a key step with 30% yield on gram-scale. Additionally, the reaction mechanism involving chloride cation was proposed based on some preliminary control experiments. (Figure presented.).
- Tang, Shi-Zhong,Zhao, Wenshuang,Chen, Tao,Liu, Yang,Zhang, Xiao-Ming,Zhang, Fu-Min
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supporting information
p. 4177 - 4183
(2017/12/18)
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